Na+ channel block prevents the ischemia-induced release of norepinephrine from spinal cord slices

1998 ◽  
Vol 346 (2-3) ◽  
pp. 145-150 ◽  
Author(s):  
Yoshitaka Uchihashi ◽  
Agnes Bencsics ◽  
Eiichiro Umeda ◽  
Tetsuji Nakai ◽  
Tetsuo Sato ◽  
...  
Keyword(s):  
Spinal Cord ◽  
Na Channel ◽  
Channel Block

Glial cells have heart: rH1 Na+ channel mRNA and protein in spinal cord astrocytes

Glia ◽  
1998 ◽  
Vol 23 (3) ◽  
pp. 200-208 ◽  
Author(s):  
J.A. Black ◽  
S. Dib-Hajj ◽  
S. Cohen ◽  
A.W. Hinson ◽  
S.G. Waxman
Keyword(s):  
Spinal Cord ◽  
Glial Cells ◽  
Na Channel

scholarly journals Block of Neuronal Na+Channels by Antidepressant Duloxetine in a State-dependent Manner

2010 ◽  
Vol 113 (3) ◽  
pp. 655-665 ◽  
Author(s):  
Sho-Ya Wang ◽  
Joanna Calderon ◽  
Ging Kuo Wang
Keyword(s):  
Open Channel ◽  
Site Directed Mutagenesis ◽  
Na Channel ◽  
Dependent Manner ◽  
Channel Block ◽  
Na Channels ◽  
Patch Clamp Technique ◽  
Open Channel Block ◽  
Human Embryonic Kidney Cells ◽  
Na Currents

Background Duloxetine is a mixed serotonin-norepinephrine reuptake inhibitor used for major depressive disorder. Duloxetine is also beneficial for patients with diabetic peripheral neuropathy and with fibromyalgia, but how it works remains unclear. Methods We used the whole cell, patch clamp technique to test whether duloxetine interacts with the neuronal Nav1.7 Na+ channel as a potential target. Resting and inactivated Nav1.7 Na+ channel block by duloxetine were measured by conventional pulse protocols in transfected human embryonic kidney cells. The open-channel block was determined directly using inactivation-deficient mutant Nav1.7 Na+ channels. Results The 50% inhibitory concentration (IC50) of duloxetine for the resting and inactivated wild-type hNav1.7 Na+ channel were 22.1+/-0.4 and 1.79+/-0.10 microM, respectively (mean+/-SE, n=5). The IC50 for the open Na+ channel was 0.25+/-0.02 microM (n=5), as determined by the block of persistent late Nav1.7 Na+ currents. Similar open-channel block by duloxetine was found in the muscle Nav1.4 isoform (IC50=0.51+/-0.05 microM; n=5). Block by duloxetine appeared via the conserved local anesthetic receptor as determined by site-directed mutagenesis. Finally, duloxetine elicited strong use-dependent block of neuronal transient Nav1.7 Na+ currents during repetitive stimulations. Conclusions Duloxetine blocks persistent late Nav1.7 Na+ currents preferentially, which may in part account for its analgesic action.

scholarly journals A human muscle Na+channel mutation in the voltage sensor IV/S4 affects channel block by the pentapeptide KIFMK

1999 ◽  
Vol 518 (1) ◽  
pp. 13-22 ◽  
Author(s):  
W. Peter ◽  
N. Mitrovic ◽  
M. Schiebe ◽  
F. Lehmann-Horn ◽  
H. Lerche
Keyword(s):  
Human Muscle ◽  
Voltage Sensor ◽  
Na Channel ◽  
Channel Block ◽  
Channel Mutation
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